BR9915475A - Derivados da quinolina-4-carboxamida comoantagonistas dos receptores de nk-3 e nk-2 - Google Patents

Derivados da quinolina-4-carboxamida comoantagonistas dos receptores de nk-3 e nk-2

Info

Publication number
BR9915475A
BR9915475A BR9915475-7A BR9915475A BR9915475A BR 9915475 A BR9915475 A BR 9915475A BR 9915475 A BR9915475 A BR 9915475A BR 9915475 A BR9915475 A BR 9915475A
Authority
BR
Brazil
Prior art keywords
alkyl
optionally substituted
aryl
group
cycloalkyl
Prior art date
Application number
BR9915475-7A
Other languages
English (en)
Inventor
Carlo Farina
Giuseppe Giardina
Mario Grugni
Marcel Morvan
Guy Marguerite Marie Gerard Nadler
Luca Francesco Raveglia
Original Assignee
Smithkline Beecham Spa
Smithkline Beecham Lab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB9825553.2A external-priority patent/GB9825553D0/en
Priority claimed from GBGB9825552.4A external-priority patent/GB9825552D0/en
Application filed by Smithkline Beecham Spa, Smithkline Beecham Lab filed Critical Smithkline Beecham Spa
Publication of BR9915475A publication Critical patent/BR9915475A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/50—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4
    • C07D215/52—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4 with aryl radicals attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Nutrition Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

"DERIVADOS DA QUINOLINA-4-CARBOXAMIDA COMOANTAGONISTAS DOS RECEPTORES DE NK-3 E NK-2".Trata-se de um composto, ou um solvato ou um sal delesproveniente, de fórmula (I): onde, Ar é um grupo arila ou um grupocicloalcadienila C~ 5-7~ opcionalmente substituídos, ou um grupocicloalquila C~ 5-7~ OPcionalmente substituído, ou um grupoaromático heterocíclico de anel único ou fundido opcionalmentesubstituído; R é hidrogênio, alquila C~ 1-6~, cicloalquila C~ 3-7~,cicloalquilalquila C~ 3-7~, lineares ou ramificadas; R~ 1~,representa hidrogênio ou até três substituíntes opcionaisselecionados a partir da lista consistindo de: alquila C~ 1-6~,alquenila C~ 1-6~, arila, alcoxila C~ 1-6~, hidroxila, halogênio, nitro,ciano, carboxila, carboxamido, sulfonamido, alcoxicarbonila C~1-6~, trifluorometila, aciloxila, amino ou mono- e di-alquilamino C~1-6~; R~ 2~ representa uma fração -(CH~ 2~)~ n~-NY~ 1~Y~ 2~onde n é um inteiro na faixa de 1 a 9, Y~ 1~ e Y~ 2~ sãoindependentemente selecionados a partir de alquila C~ 1-6~;alquila C~ 1-6~ substituída com hidroxila, alcoxila, alquilamino C~1-6~ ou bis (alquil C~ 1-6~) amino; cicloalquila C~ 3-6~;azobicicloalquila C~ 4-6~; alquenila C~ 1-6~; arila ou aril-alquila-C~1-6~ ou Y~ 1~ e Y~ 2~ juntamente com o átomo de nitrogênio aoqual eles estão ligados representam um grupo heterocíclico deanel único ou fundido N-articulado opcionalmente substituído; R~3~ é alquila C~ 1-6~, cicloalquila C~ 3-7~, cicloalquilalquila C~4-7~, lineares ou ramificadas, arila opcionalmente substituída, ouum grupo aromático heterocíclico de anel único ou fundidoopcionalmente substituído; e R~ 4~ representa hidrogênio oualquila C~ 1-6~; R~ 5~ representa hidrogênio ou halogênio; umprocesso para a preparação de tais compostos, uma composiçãofarmacêutica contendo tais compostos e o uso de tais compostos ecomposições em medicina.
BR9915475-7A 1998-11-20 1999-11-19 Derivados da quinolina-4-carboxamida comoantagonistas dos receptores de nk-3 e nk-2 BR9915475A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9825553.2A GB9825553D0 (en) 1998-11-20 1998-11-20 Novel Compounds
GBGB9825552.4A GB9825552D0 (en) 1998-11-20 1998-11-20 Novel compounds
PCT/EP1999/009115 WO2000031037A1 (en) 1998-11-20 1999-11-19 Quinoline-4-carboxamide derivatives as nk-3 and nk-2 receptor antagonists

Publications (1)

Publication Number Publication Date
BR9915475A true BR9915475A (pt) 2001-12-18

Family

ID=26314705

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9915475-7A BR9915475A (pt) 1998-11-20 1999-11-19 Derivados da quinolina-4-carboxamida comoantagonistas dos receptores de nk-3 e nk-2

Country Status (18)

Country Link
EP (1) EP1131295A1 (pt)
JP (1) JP2002530377A (pt)
KR (1) KR20010075726A (pt)
CN (1) CN1406225A (pt)
AR (2) AR021355A1 (pt)
AU (1) AU768708B2 (pt)
BR (1) BR9915475A (pt)
CA (1) CA2351865A1 (pt)
CO (1) CO5150149A1 (pt)
HK (1) HK1041257A1 (pt)
HU (1) HUP0104959A3 (pt)
IL (1) IL143137A0 (pt)
MX (1) MXPA01005095A (pt)
NO (1) NO20012473L (pt)
NZ (1) NZ511777A (pt)
PL (1) PL347721A1 (pt)
TR (1) TR200101412T2 (pt)
WO (1) WO2000031037A1 (pt)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7037922B1 (en) 2000-03-10 2006-05-02 Neurogen Corporation Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands
GB0027701D0 (en) * 2000-11-13 2000-12-27 Smithkline Beecham Spa Novel compounds
JP2004517062A (ja) * 2000-11-13 2004-06-10 グラクソスミスクライン・ソシエタ・ペル・アチオニ Ｎｋ−３およびｎｋ−２アンタゴニストとしてのキノリン誘導体
GB0028964D0 (en) * 2000-11-28 2001-01-10 Smithkline Beecham Spa Novel compounds
AU2002226356A1 (en) * 2000-11-28 2002-06-11 Glaxosmithkline S.P.A. Quinoline derivatives as nk-3 antagonists
WO2002043734A1 (en) * 2000-11-28 2002-06-06 Glaxosmithkline Spa Novel compounds
MXPA03009239A (es) 2001-04-10 2004-11-12 Johnson & Johnson Derivados de 1,3,8-triazapiro[4,5]decan-4-ona utiles para el tratamiento de trastornos mediados por el receptor orl-1.
GB0109122D0 (en) * 2001-04-11 2001-05-30 Smithkline Beecham Spa Novel compounds
EP1659120A1 (en) * 2001-04-11 2006-05-24 GlaxoSmithKline S.p.A. 3-substituted quinoline-4-carboxamide derivatives as NK-3 and NK-2 receptor antagonists
MY134211A (en) * 2001-05-18 2007-11-30 Smithkline Beecham Corp Novel use
EP1541149A1 (en) * 2002-06-26 2005-06-15 Kyowa Hakko Kogyo Co., Ltd. Phosphodiesterase inhibitor
WO2004022558A2 (en) 2002-09-09 2004-03-18 Janssen Pharmaceutica, N.V. Hydroxy alkyl substituted 1,3,8-triazaspiro[4.5]decan-4-one derivatives useful for the treatment of orl-1 receptor mediated disorders
GB0303086D0 (en) 2003-02-11 2003-03-19 Merck Sharp & Dohme New compounds
WO2005000247A2 (en) * 2003-06-25 2005-01-06 Smithkline Beecham Corporation 4-carboxamido quinoline derivatives for use as nk-2 and nk-3
GB0419192D0 (en) 2004-08-27 2004-09-29 Merck Sharp & Dohme Therapeutic agents
GB0425076D0 (en) * 2004-11-12 2004-12-15 Smithkline Beecham Corp Novel compounds
GB0509405D0 (en) * 2005-05-10 2005-06-15 Merck Sharp & Dohme Therapeutic compounds
KR20080016591A (ko) * 2005-06-03 2008-02-21 아스트라제네카 아베 Ｎｋ3 길항제로서의 퀴놀린 유도체
GB0515580D0 (en) 2005-07-29 2005-09-07 Merck Sharp & Dohme Therapeutic compounds
AR057130A1 (es) 2005-09-21 2007-11-14 Astrazeneca Ab Quinolinas de alquilsulfoxido y una composicion farmaceutica
WO2007039123A2 (en) * 2005-09-22 2007-04-12 Smithkline Beecham Corporation Combination therapy comprising an nk-3 antagonist and an antipsychotic agent
TW201018662A (en) * 2005-12-12 2010-05-16 Astrazeneca Ab Alkylsulphonamide quinolines
WO2008016006A1 (en) * 2006-07-31 2008-02-07 Ono Pharmaceutical Co., Ltd. Compound having cyclic group bound thereto through spiro binding and use thereof
WO2008067167A1 (en) 2006-11-28 2008-06-05 Janssen Pharmaceutica N.V. Salts of 3-(3-amino-2-(r)-hydroxy-propyl)-1-(4-fluoro-phenyl)-8-(8-methyl-naphthalen-1-ylmethyl)-1,3,8-triaza-spiro[4.5]decan-4-one
WO2008097976A1 (en) * 2007-02-09 2008-08-14 Kalypsys, Inc. Heterocyclic modulators of tgr5 for treatment of disease
CN101679430B (zh) 2007-04-09 2013-12-25 詹森药业有限公司 用于治疗焦虑和抑郁症的作为orl-1受体的配体的1,3,8-三取代-1,3,8-三氮杂-螺[4.5]癸-4-酮衍生物
ES2561674T3 (es) * 2010-03-23 2016-02-29 Glaxosmithkline Llc Antagonistas de TRPV4
CA2909752A1 (en) 2013-04-19 2014-10-23 Astrazeneca Ab A nk3 receptor antagonist compound (nk3ra) for use in a method for the treatment of polycystic ovary syndrome (pcos)
WO2017072629A1 (en) 2015-10-29 2017-05-04 Cadila Healthcare Limited Pharmaceutical combination of nk3 receptor antagonist and biguanides

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ291476B6 (cs) * 1994-05-27 2003-03-12 Smithkline Beecham S. P. A. N-(alfa-Ethylbenzyl)-3-hydroxy-2-fenylchinolin-4-karboxamid, farmaceutický prostředek s jeho obsahem a použití
AR004735A1 (es) * 1995-11-24 1999-03-10 Smithkline Beecham Spa Quinoleina 4-amido sustituida, un procedimiento para su preparacion, una composicion farmaceutica que los contiene y el uso de los mismos para lapreparacion de un medicamento.
BR9809652A (pt) * 1997-05-23 2001-09-11 Smithkline Beecham Spa Derivados de quinolina-4-carboxamida como antagonistas de receptor nk-2 e nk-3

Also Published As

Publication number Publication date
PL347721A1 (en) 2002-04-22
TR200101412T2 (tr) 2001-10-22
NO20012473L (no) 2001-07-18
CN1406225A (zh) 2003-03-26
AU1777000A (en) 2000-06-13
HUP0104959A3 (en) 2003-01-28
HUP0104959A2 (hu) 2002-04-29
AU768708B2 (en) 2004-01-08
NZ511777A (en) 2003-12-19
AR021354A1 (es) 2002-07-17
KR20010075726A (ko) 2001-08-09
HK1041257A1 (zh) 2002-07-05
EP1131295A1 (en) 2001-09-12
JP2002530377A (ja) 2002-09-17
IL143137A0 (en) 2002-04-21
CA2351865A1 (en) 2000-06-02
WO2000031037A1 (en) 2000-06-02
MXPA01005095A (es) 2002-04-24
CO5150149A1 (es) 2002-04-29
AR021355A1 (es) 2002-07-17
NO20012473D0 (no) 2001-05-18

Similar Documents

Publication Publication Date Title
BR9915475A (pt) Derivados da quinolina-4-carboxamida comoantagonistas dos receptores de nk-3 e nk-2
BR9809652A (pt) Derivados de quinolina-4-carboxamida como antagonistas de receptor nk-2 e nk-3
BR0307409A (pt) Compostos de hidrazida de ácido 2-furanocarboxìlico, composições farmacêuticas contendo os mesmos e uso dos mesmos para preparação de um agente preventivo ou terapêutico
EA200000334A1 (ru) Производные карбоксамидотиазолов, их получение, содержащие их фармацевтические композиции
AR040031A1 (es) Compuestos de pirazol-pirimidina anilina utiles como inhibidores de cinasa y composiciones farmaceuticas que los contienen
BR0111754A (pt) Uso de um composto, método para inibir aurora 2 quinase em um animal de sangue quente, composto, e, composição farmacêutica
EA200200942A1 (ru) Фармацевтические композиции, содержащие производные 3-аминоазетидина, новые производные и способ их получения
AR004219A1 (es) Nuevos derivados de quinazolina, procedimientos para su preparacion, composiciones que los contienen y su uso en la preparacion de medicamentos,particularmente en el tratamiento de trastornos inflamatorios
ES2088933T3 (es) Derivados de pirazol, procedimientos para su preparacion y composicion farmaceutica que los contiene.
EA200000842A1 (ru) Бицикло [2.2.1] гептаны и родственные соединения
AR004972A1 (es) Compuesto quinolino 4-carboxamidas n-sustituidas, un procedimiento para su preparacion, el uso de los mismos para la fabricacion de un medicamento, una composicion farmaceutica y un antagonista nk-2/nk-3 combinado.
DK0528337T3 (da) Thiazolylbenzofuranderivater, fremgangsmåde til fremstilling deraf og farmaceutiske præparater, der indeholder disse forbin
MXPA03011638A (es) Nuevos derivados de 4-piperazinil indol con afinidad por el receptor 5-ht6.
ATE556058T1 (de) 1-(2h)-isochinolonderivat
DK1106612T3 (da) Quinolinderivater, der er nyttige til inhibering af farnesylproteintransferase
IL184687A0 (en) Pharmaceutical compositions containing 1,2-dihydropyridin-2-one derivatives
BR9911013A (pt) Derivados de pirazol como inibidores da p-38 map quinase
EA200200912A1 (ru) Новые производные индолин-2-она, их получение и их применение в качестве лигандов рецепторов окситоцина
ES2174298T3 (es) Derivados de aminotiazol, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen.
HUP0302193A2 (hu) 1,4-Diazabiciklo[3.2.2]nonán-benzoxazol,-benzotiazol és -benzimidazol-származékok, előállításuk és ezeket tartalmazó gyógyszerkészítmények
EA200100090A2 (ru) Новые пиперидин-4-сульфонамидные производные, способ их получения и содержащие их фармацевтические композиции
DE69934514D1 (de) Chinolinderivate als nk-2 und nk-3 rezeptor-liganden
ID23954A (id) Tetrahidrogama-karbolin
HUP0203332A2 (hu) Ciklotiokarbamát-származékok, progeszteron receptor modulátorokként való alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
HUP0203603A2 (hu) Új IL-8 receptor antagonista hatású indolszármazékok és ezeket tartalmazó gyógyszerkészítmények

Legal Events

Date Code Title Description
TC Change of name
TE Change of address
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 6O, 7O E 8O ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 1913 DE 04/09/2007.